Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery

Abstract A widely established prodrug strategy can effectively optimize the unappealing properties of therapeutic agents in cancer treatment. Among them, lipidic prodrugs extremely uplift the physicochemical properties, site-specificity, and antitumor activities of therapeutic agents while reducing...

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Main Authors: Lingling Huang, Jianmiao Yang, Tiantian Wang, Jianqing Gao, Donghang Xu
Format: Article
Language:English
Published: BMC 2022-01-01
Series:Journal of Nanobiotechnology
Subjects:
Online Access:https://doi.org/10.1186/s12951-022-01257-4
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author Lingling Huang
Jianmiao Yang
Tiantian Wang
Jianqing Gao
Donghang Xu
author_facet Lingling Huang
Jianmiao Yang
Tiantian Wang
Jianqing Gao
Donghang Xu
author_sort Lingling Huang
collection DOAJ
description Abstract A widely established prodrug strategy can effectively optimize the unappealing properties of therapeutic agents in cancer treatment. Among them, lipidic prodrugs extremely uplift the physicochemical properties, site-specificity, and antitumor activities of therapeutic agents while reducing systemic toxicity. Although great perspectives have been summarized in the progress of prodrug-based nanoplatforms, no attention has been paid to emphasizing the rational design of small-molecule lipidic prodrugs (SLPs). With the aim of outlining the prospect of the SLPs approach, the review will first provide an overview of conjugation strategies that are amenable to SLPs fabrication. Then, the rational design of SLPs in response to the physiological barriers of chemotherapeutic agents is highlighted. Finally, their biomedical applications are also emphasized with special functions, followed by a brief introduction of the promising opportunities and potential challenges of SLPs-based drug delivery systems (DDSs) in clinical application. Graphical Abstract
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spelling doaj.art-ed08acb75a284ceab255a834cdfbcd9f2022-12-22T04:19:50ZengBMCJournal of Nanobiotechnology1477-31552022-01-0120111510.1186/s12951-022-01257-4Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug deliveryLingling Huang0Jianmiao Yang1Tiantian Wang2Jianqing Gao3Donghang Xu4Department of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of MedicineTaizhou Hospital of Zhejiang ProvinceDepartment of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of MedicineZhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang UniversityDepartment of Pharmacy, The Second Affiliated Hospital, Zhejiang University School of MedicineAbstract A widely established prodrug strategy can effectively optimize the unappealing properties of therapeutic agents in cancer treatment. Among them, lipidic prodrugs extremely uplift the physicochemical properties, site-specificity, and antitumor activities of therapeutic agents while reducing systemic toxicity. Although great perspectives have been summarized in the progress of prodrug-based nanoplatforms, no attention has been paid to emphasizing the rational design of small-molecule lipidic prodrugs (SLPs). With the aim of outlining the prospect of the SLPs approach, the review will first provide an overview of conjugation strategies that are amenable to SLPs fabrication. Then, the rational design of SLPs in response to the physiological barriers of chemotherapeutic agents is highlighted. Finally, their biomedical applications are also emphasized with special functions, followed by a brief introduction of the promising opportunities and potential challenges of SLPs-based drug delivery systems (DDSs) in clinical application. Graphical Abstracthttps://doi.org/10.1186/s12951-022-01257-4CancerSmall moleculeLipidic prodrugNanomedicineDrug delivery
spellingShingle Lingling Huang
Jianmiao Yang
Tiantian Wang
Jianqing Gao
Donghang Xu
Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
Journal of Nanobiotechnology
Cancer
Small molecule
Lipidic prodrug
Nanomedicine
Drug delivery
title Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
title_full Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
title_fullStr Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
title_full_unstemmed Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
title_short Engineering of small-molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
title_sort engineering of small molecule lipidic prodrugs as novel nanomedicines for enhanced drug delivery
topic Cancer
Small molecule
Lipidic prodrug
Nanomedicine
Drug delivery
url https://doi.org/10.1186/s12951-022-01257-4
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AT tiantianwang engineeringofsmallmoleculelipidicprodrugsasnovelnanomedicinesforenhanceddrugdelivery
AT jianqinggao engineeringofsmallmoleculelipidicprodrugsasnovelnanomedicinesforenhanceddrugdelivery
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